Preclinical developments in antiobesity drugs

Appetite and Body Weight

Volumn , Issue , 2007, Pages 323-336

  Vickers, Steven P ^a   Cheetham, Sharon C ^a  

^a RenaSci Ltd   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 43549093795     PISSN: None     EISSN: None     Source Type: Book    
DOI: 10.1016/B978-012370633-1/50013-X     Document Type: Chapter

References (81)

1. Alberts P., Nilsson C., Selen G., Engblom L.O., Edling N.H., Norling S., Klingstrom G., Larsson C., Forsgren M., Ashkzari M., Nilsson C.E., Fiedler M., Bergqvist E., Ohman B., Bjorkstrand E., Abrahmsen L.B. Selective inhibition of 11 beta-hydroxysteroid dehydrogenase type 1 improves hepatic insulin sensitivity in hyperglycemic mice strains. Endocrinology 2003, 144:4755-4762.
2. Antel J., Hebebrand J., Preuschoff U., David S., Sann H., Weske M. Method for locating compounds which are suitable for the treatment and/or prophylaxis of obesity 2002, WO Patent 0207821.
3. Arch J.R.S., Wang S.J.Y., Birtles S., Smith D.M., Turnbull A. Effects of an inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 inhibitor on energy balance and glucose homeostasis in diet-induced obesity. Diabetologia 2005, 48(Suppl 1):A238. Abstract 650.
4. Astrup A., Caterson I., Zelissen P., Guy-Grand B., Carruba M., Levy M., Sun X., Fitchet M. Topiramate: Long-term maintenance of weight-loss induced by a low-calorie diet in obese subjects. Obes. Res. 2004, 12:1658-1669.
5. Batterham R.L., Cowley M.A., Small C.J., Herzog H., Cohen M.A., Dakin C.L., Wren A.M., Brynes A.E., Low M.J., Ghatei M.A., Cone R.D., Bloom S.R. Gut hormone PYY(3-36) physiologically inhibits food intake. Nature 2002, 418:650-654.
6. Bensaid M., Gary-Bobo M., Esclangon A., Maffrand J.P., Le Fur G., Oury-Donat F., Soubrié P. The cannabinoid CB1 receptor antagonist SR141716 increases Acrp30 mRNA expression in adipose tissue of obese fa/fa rats and in cultured adipocyte cells. Mol. Pharmacol. 2003, 63:908-914.
7. Bentley J.C., Marsden C.A., Sleight A.J., Fone K.C.F. Effect of the 5-HT6 antagonist, Ro 046790 on food consumption in rats trained to a fixed feeding regime. Br. J. Pharmacol. 1999, 126. 66P.
8. Bickerdike M.J., Vickers S.P., Dourish C.T. 5-HT2C receptor modulation and the treatment of obesity. Diabetes Obes. Metab. 1999, 1:207-214.
9. Bittencourt J.C., Presse F., Arias C., Peto C., Vaughan J., Nahon J.L., Vale W., Sawchenko P.E. The melanin-concentrating hormone system of the rat brain: an immuno- and hybridization histochemical characterization. J. Comp. Neurol. 2002, 319(2):218-245.
10. Black S.C. Cannabinoid receptor antagonists and obesity. Curr. Opin. Invest. Drugs 2004, 5:389-394.
11. Boggiano M.M., Chandler P.C., Oswald K.D., Rodgers R.J., Blundell J.E., Ishii Y., Beattie A.H., Holch P., Allison D.B., Schindler M., Arndt K., Rudolf K., Mark M., Schoelch C., Joost H.G., Klaus S., Thone-Reineke C., Benoit S.C., Seeley R.J., Beck-Sickinger A.G., Koglin N., Raun K., Madsen K., Wulff B.S., Stidsen C.E., Birringer M., Kreuzer O.J., Deng X.Y., Whitcomb D.C., Halem H., Taylor J., Dong J., Datta R., Culler M., Ortmann S., Castaneda T.R., Tschop M. PYY3-36 as an anti-obesity drug target. Obes. Rev. 2005, 6:307-322.
12. Bohlooly Y.M., Mahlapuu M., Andersen H., Astrand A., Hjorth S., Svensson L., Tornell J., Snaith M.R., Morgan D.G., Ohlsson C. Osteoporosis in MCHR1-deficient mice. Biochem. Biophys. Res. Commun. 2004, 318:964-969.
13. Bonow R.O., Eckel R.H. Diet, obesity and cardiovascular risk. N. Engl. J. Med. 2003, 348:2057-2058.
14. Borowsky B., Durkin M.M., Ogozalek K., Marzabadi M.R., DeLeon J., Lagu B., Heurich R., Lichtblau H., Shaposhnik Z., Daniewska I., Blackburn T.P., Branchek T.A., Gerald C., Vaysse P.J., Forray C. Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist. Nat. Med. 2002, 8:825-830.
15. Bray G.A., Hollander P., Klein S., Kushner R., Levy B., Fitchet M., Perry B.H. A 6-month randomized, placebo-controlled, dose-ranging trial of topiramate for weight loss in obesity. Obes. Res. 2003, 11:722-733.
16. 6, receptor antagonism, a novel mechanism for the management of obesity. SMi Conf Obesity and Related Disorders 2003.
17. 6 receptor antagonist(s) for the treatment of obesity. Neuropsychopharmacology 2005, 30(Suppl. 1):S54.
18. Collins C.A., Kym P.R. Prospects for obesity treatment: MCH receptor antagonists. Curr. Opin. Invest. Drugs 2003, 4:386-394.
19. Colombo G., Agabio R., Diaz G., Lobina C., Reali R., Gessa G.L. Appetite suppression and weight loss after the cannabinoid antagonist SR 141716. Life Sci. 1998, 63:113-117.
20. Despres J.P., Golay A., Sjostrom L. Rimonabant in Obesity-Lipids Study Group. Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemia. N. Engl. J. Med. 2005, 353:2121-2134.
21. Dyke H.J., Ray N.C. Recent developments in the discovery of MCH-1R antagonists for the treatemnt of obesity-an update. Expert Opin. Ther. Patents 2005, 15:1303-1313.
22. Edwards C.M. The GLP-1 system as a therapeutic target. Ann. Med. 2005, 37:314-322.
23. Fan W., Boston B.A., Kesterson R.A., Hruby V.J., Cone R.D. Role of melanocortinergic neurons in feeding and the agouti obesity syndrome. Nature 1997, 385:165-168.
24. Feletou M., Levens N.R. Neuropeptide Y2 receptors as drug targets for the central regulation of body weight. Curr. Opin. Invest. Drugs 2005, 6:1002-1011.
25. Foltin R.W., Fischman M.W., Byrne M.F. Effects of smoked marijuana on food intake and body weight of humans living in a residential laboratory. Appetite 1988, 11:1-14.
26. Fontaine K.R., Redden D.T., Wang C., Westfall A.O., Allison D.B. Years of life lost due to obesity. JAMA 2003, 289:187-193.
27. Gary-Bobo M., Elachouri G., Scatton B., Le Fur G., Oury-Donat F., Bensaid M. The cannabinoid CB1 receptor antogonist rimonabant (SR141716) inhibits cell proliferation and increases markers of adipocyte maturation in cultured mouse 3T3 F442A preadipocytes. Mol. Pharmacol. 2006, 69:471-478.
28. Gobbi G., Bambico F.R., Mangieri R., Bortolato M., Campolongo P., Solinas M., Cassano T., Morgese M.G., Debonnel G., Duranti A., Tontini A., Tarzia G., Mor M., Trezza V., Goldberg S.R., Cuomo V., Piomelli D. Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis. Proc. Natl. Acad. Sci. U.S.A. 2005, 102:18620-18625.
29. Gomez R., Navarro M., Ferrer B., Trigo J.M., Bilbao A., Del Arco I., Cippitelli A., Nava F., Piomelli D., Rodriguez de Fonseca F. A peripheral mechanism for CB1 cannabinoid receptor-dependent modulation of feeding. J. Neurosci. 2002, 22(21):9612-9617.
30. Goodfellow V.S., Saunders J. The melanocortin system and its role in obesity and cachexia. Curr. Top. Med. Chem. 2003, 3:855-883.
31. Gordon A., Price H. Mood stabilisation and weight loss with topiramate. Am. J. Psychiatry 1999, 156:968-969.
32. Hirst W.D., Abrahamsen B., Blaney F.E., Calver A.R., Aloj L., Price G.W., Medhurst A.D. Differences in the central nervous system distribution and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand binding, site-directed mutagenesis, and molecular modeling. Mol. Pharmacol. 2003, 64:1295-1308.
33. Horvath T.L. The hardship of obesity: a softwired hypothalamus. Nature Neurosci. 2005, 8:561-565.
34. Hoyer D., Hannon J.P., Martin G.R. Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol. Biochem. Behav. 2002, 71:533-554.
35. Huszar D., Lynch C.A., Fairchild-Huntress V., Dunmore J.H., Fang Q., Berkemeier L.R., Gu W., Kesterson R.A., Boston B.A., Cone R.D., Smith F.J., Campfield L.A., Burn P., Lee F. Targeted disruption of the melanocortin-4 receptor results in obesity in mice. Cell 1997, 88:131-141.
36. King P.J. The hypothalamus and obesity. Curr. Drug Targets 2005, 6:225-240.
37. Kirkham T.C. Endocannabinoids in the regulation of appetite and body weight. Behav. Pharmacol. 2005, 16:297-313.
38. Kirkham T.C., Williams C.M. Endogenous cannabinoids and appetite. Nutr. Res. Rev. 2001, 14:65-86.
39. Kirkham T.C., Williams C.M. Endocannabinoid receptor antagonists: potential for obesity treatment. Trent. Endocrinol. 2004, 3:345-360.
40. Kowalski T.J., McBriar M.D. Therapeutic potential of melanin-concentrating hormone-1 receptor antagonists for the treatment of obesity. Expert Opin. Invest. Drugs 2004, 13:1113-1122.
41. Lobstein T., Baur L., Uauy R. Obesity in children and young people. A crisis in public health. Obes. Rev. 2004, 5(Suppl.):4-104.
42. Lynch C.J., Fox H., Hazen S.A., Stanley B.A., Dodgson S.J., Lanoue K.F. Role of hepatic carbonic anhydrase in de novo lipogenesis. Biochem. J. 1995, 310:197-202.
43. Masuzaki H., Paterson J., Shinyama H., Morton N.M., Mullins J.J., Seckl J.R., Flier J.S. A transgenic model of visceral obesity and the metabolic syndrome. Science 2001, 294:2166-2170.
44. National Audit Office, U.K. Controller and Auditor General. Tackling Obesity in England 2001, The Stationary Office, London.
45. O'Rahilly S., Yeo G.S., Farooqi I.S. Melanocortin receptors weigh in. Nat. Med. 2004, 10:351-352.
46. Pendharkar V.V., Vishwakarma S.L., Patel A.S., Shrisath V.S., Kambhampati S.R., Nirogi V.S. Effect of selective 5-HT receptor antagonists on food intake, and body weight gain. Soc. Neurosci. Abstr. 2005, P533.7.
47. Pi-Sunyer F., Aronne L., Heshmati H., Devin J., Rosenstock J. Effect of rimonabant, a cannabinoid-1 receptor blocker, on weight and cardiometabolic risk factors in overweight or obese patients. RIO-North America: a randomized controlled trial. JAMA 2006, 295:761-775.
48. Qu D., Ludwig D.S., Gammeltoft S., Piper M., Pelleymounter M.A. A role for melanin-concentrating hormone in the central regulation of feeding behaviour. Nature 1996, 380:243-247.
49. Ravinet-Trillou C., Arnone M., Delgorge C., Gonalons N., Keane P., Maffrand J.P., Soubrie P. Anti-obesity effect of SR141716, a CB1 receptor antagonist, in diet-induced obese mice. Am. J. Physiol. Regul. Integr. Comp. Physiol. 2003, 284:R345-R353.
50. Ravinet-Trillou C., Delgorge C., Menet C., Arnone M., Soubrie P. CB1 cannabinoid receptor knockout in mice leads to leanness, resistance to diet-induced obesity and enhanced leptin sensitivity. Int. J. Obes. Relat. Metab. Disord. 2004, 28:640-648.
51. Rinaldi-Carmona M., Barth F., Heaulme M., Shire D., Calandra B., Congy C., Martinez S., Maruani J., Neliat G., Caput D. SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett. 1994, 350:240-244.
52. Ristic S., Byiers S., Foley J., Holmes D. Improved glycaemic control with dipeptidyl peptidase-4 inhibition in patients with type 2 diabetes: vildagliptin (LAF237) dose response. Diabetes Obes. Metab. 2005, 7:692-698.
53. Rossi M., Beak S.A., Choi S.J., Small C.J., Morgan D.G., Ghatei M.A., Smith D.M., Bloom S.R. Investigation of the feeding effects of melanin concentrating hormone on food intake-action independent of galanin and the melanocortin receptors. Brain Res. 1999, 846:164-170.
54. Sainsbury A., Schwarzer C., Couzens M., Fetissov S., Furtinger S., Jenkins A., Cox H.M., Sperk G., Hokfelt T., Herzog H. Important role of hypothalamic Y2 receptors in body weight regulation revealed in conditional knockout mice. Proc. Natl. Acad. Sci. U.S.A. 2002, 99:8938-8943.
55. Sainsbury A., Baldock P.A., Schwarzer C., Ueno N., Enriquez R.F., Couzens M., Inui A., Herzog H., Gardiner E.M. Synergistic effects of Y2 and Y4 receptors on adiposity and bone mass revealed in double knockout mice. Mol. Cell. Biol. 2003, 23:5225-5233.
56. Sainsbury A., Bergen H.T., Boey D., Bamming D., Cooney G.J., Lin S., Couzens M., Stroth N., Lee N.J., Lindner D., Singewald N., Karl T., Duffy L., Enriquez R., Slack K., Sperk G., Herzog H. Y2Y4 receptor double knockout protects against obesity due to a high-fat diet or Y1 receptor deficiency in mice. Diabetes 2006, 55:19-26.
57. Setola V., Roth B.L. Why mice are neither miniature humans nor small rats: a cautionary tale involving 5-hydroxytryptamine-6 serotonin receptor species variants. Mol. Pharmacol. 2003, 64:1277-1278.
58. Shearman L.P., Camacho R.E., Sloan Stribling D., Zhou D., Bednarek M.A., Hreniuk D.L., Feighner S.D., Tan C.P., Howard A.D., Van der Ploeg L.H., MacIntyre D.E., Hickey G.J., Strack A.M. Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats. Eur. J. Pharmacol. 2003, 475:37-47.
59. Shimada M., Tritos N.A., Lowell B.B., Flier J.S., Maratos-Flier E. Mice lacking melanin-concentrating hormone are hypophagic and lean. Nature 1998, 396:670-674.
60. Skofitsch G., Jacobowitz D.M., Zamir N. Immunohistochemical localization of a melanin concentrating hormone-like peptide in the rat brain. Brain Res. Bull. 1985, 15:635-649.
61. Sleight A.J., Boess F.G., Bos M., Levet-Trafit B., Riemer C., Bourson A. Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors. Br. J. Pharmacol. 1998, 124:556-562.
62. Supuran C.T. Carbonic anhydrase inhibitors in the treatment and prophylaxis of obesity. Exp. Opin. Ther. Patents 2003, 13:1545-1550.
63. Tan C.P., Sano H., Iwaasa H., Pan J., Sailer A.W., Hreniuk D.L., Feighner S.D., Palyha O.C., Pong S.S., Figueroa D.J., Austin C.P., Jiang M.M., Yu H., Ito J., Ito M., Ito M., Guan X.M., MacNeil D.J., Kanatani A., Van der Ploeg L.H., Howard A.D. Melanin-concentrating hormone receptor subtypes 1 and 2: species-specific gene expression. Genomics 2002, 79:785-792.
64. Tschop M., Smiley D.L., Heiman M.L. Ghrelin induces adiposity in rodents. Nature 2000, 407:908-913.
65. Turnbull A.V., Ellershaw L., Masters D.J., Birtles S., Boyer S., Carroll D., Clarkson P., Loxham S.J., McAulay P., Teague J.L., Foote K.M., Pease J.E., Block M.H. Selective antagonism of the NPY Y5 receptor does not have a major effect on feeding in rats. Diabetes 2002, 51:2441-2449.
66. Van Gaal L.F., Rissanen A.M., Scheen A.J., Ziegler O., Rossner S. Effects of the cannabinoid-1 receptor blocker rimonabant on weight reduction and cardiovascular risk factors in overweight patients: 1-year experience from the RIO-Europe study. Lancet 2005, 365:1389-1397.
67. Vickers S.P., Dourish C.T. Serotonin receptor ligands and the treatment of obesity. Curr. Opin. Invest. Drugs 2004, 5:377-388.
68. Vickers S.P., Kennett G.A. Cannabinoids and the regulation of ingestive behaviour. Curr. Drug Targets 2005, 6:215-233.
69. Vickers S.P., Clifton P.G., Dourish C.T., Tecott L.H. Reduced satiating effect of d-fenfluramine in serotonin 5-HT(2C) receptor mutant mice. Psychopharmacology (Berlin) 1999, 143:309-314.
70. Vickers S.P., Dourish C.T., Kennett G.A. Evidence that hypophagia induced by d-fenfluramine and d-norfenfluramine in the rat is mediated by 5-HT2C receptors. Neuropharmacology 2001, 41:200-209.
71. Vickers S.P., Webster L.J., Wyatt A., Dourish C.T., Kennett G.A. Preferential effects of the cannabinoid CB1 receptor antagonist, SR 141716, on food intake and body weight gain of obese (fa/fa) compared to lean Zucker rats. Psychopharmacology (Berlin) 2003, 167:103-111.
72. Wang M. The role of glucocorticoid action in the pathophysiology of the metabolic syndrome. Nutr. Metab. (Lond.) 2005, 2:3.
73. Wilding J., Van Gaal L., Rissanen A., Vercruysse F., Fitchet M. A randomized double-blind placebo-controlled study of the long-term efficacy and safety of topiramate in the treatment of obese subjects. Int. J. Obes. 2004, 28:1399-1410.
74. Williams C.M., Kirkham T.C. Anandamide induces overeating: mediation by central cannabinoid (CB1) receptors. Psychopharmacology (Berlin) 1999, 143:315-317.
75. Williams C.M., Kirkham T.C. Reversal of delta 9-THC hyperphagia by SR141716 and naloxone but not dexfenfluramine. Pharmacol. Biochem. Behav. 2002, 71:333-340.
76. 9-THC. Physiol. Behav. 1998, 65:343-346.
77. Winum J.-Y., Scozzafaya A., Montero J.-L., Supuran C.T. Sulfamates and their therapeutic potential. Med. Res. Rev. 2005, 25(Suppl 2):186-228.
78. Wolf A.M., Colditz G.A. Current estimates of the economic costs of obesity in the United States. Obes. Res. 1998, 6:97-106.
79. Woolley M.L., Bentley J.C., Sleight A.J., Marsden C.A., Fone K.C. A role for 5-ht6 receptors in retention of spatial learning in the Morris water maze. Neuropharmacology 2001, 41:210-219.
80. Woolley M.L., Marsden C.A., Fone K.C. 5-ht6 receptors. Curr. Drug Targets CNS Neurol. Disord. 2004, 3:59-79.
81. Zhang J.V., Ren P.G., Avsian-Kretchmer O., Luo C.W., Rauch R., Klein C., Hsueh A.J. Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intake. Science 2006, 310:996-999.